Five-membered Hetero Ring Having Two Or More Ring Hetero Atoms Of Which At Least One Is Nitrogen Patents (Class 544/132)
The five-membered hetero ring has at least sulfur and nitrogen as ring hetero atoms (Class 544/133)
The five-membered hetero ring has at least oxygen and nitrogen as ring hetero atoms (Class 544/137)
1,3-diazole ring (including hydrogenated) (Class 544/139)
1,2-diazole ring (including hydrogenated) (Class 544/140)
  • 5-Aryltetrazole compounds, compositions thereof, and uses therefor
    Publication number: 20040116423
    Abstract: The present invention relates to 5-Aryltetrazole Compounds, compositions comprising an effective amount of a a 5-Aryltetrazole Compound, and methods for treating an inflammation disease, a reperfusion disease, or hyperuricemia in an animal in need thereof comprising administering to the animal an effective amount of a 5-Aryltetrazole compound.
    Type: Application
    Filed: July 17, 2003
    Publication date: June 17, 2004
    Inventors: Alex Nivorozhkin, John Van Duzer, Andrew Salzman, Garry Southan, Siya Ram, Qi Zeng, Csaba Szabo
  • New compounds
    Publication number: 20040106607
    Abstract: The present invention relates to new compounds of formula I, 1
    Type: Application
    Filed: August 8, 2003
    Publication date: June 3, 2004
    Applicant: AstraZeneca AB and NPS Pharmaceuticals, Inc.
    Inventors: Jalaj Arora, Louise Edwards, Methvin Isaac, Abdelmalik Slassi, Tomislav Stefanac, David Wensbo, Tao Xin
  • Compounds for the treatment of metabolic disorders
    Publication number: 20040092518
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Application
    Filed: October 14, 2003
    Publication date: May 13, 2004
    Inventor: Shalini Sharma
  • Substituted 3,5-diphenyl-1,2,4-triazoles and their use as pharmaceutical metal chelators
    Patent number: 6723742
    Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.
    Type: Grant
    Filed: May 29, 2003
    Date of Patent: April 20, 2004
    Assignee: Novartis AG.
    Inventors: René Lattmann, Pierre Acklin
  • Morpholine derivatives as antagonists of orexin receptors
    Publication number: 20040058921
    Abstract: This invention relates to morpholine derivatives of formula (I) and their use as antagonists of orexin receptors.
    Type: Application
    Filed: October 9, 2003
    Publication date: March 25, 2004
    Inventors: Clive Leslie Branch, Christopher Norbert Johnson, Alexander B. Smith, Geoffrey Stemp, Kevin Thewlis
  • Novel triazole derivatives, process for their preparation and pharmaceutical compositions containing them
    Publication number: 20040043995
    Abstract: The invention relates to a compound of formula 1
    Type: Application
    Filed: December 12, 2002
    Publication date: March 4, 2004
    Inventors: Eric Bignon, Jean Pierre Bras, Paul De Cointet, Pierre Despeyroux, Daniel Frehel, Danielle Gully
  • Novel aminotriazolone compounds, method for preparing same and pharmaceutical compositions containing same
    Publication number: 20040029875
    Abstract: A compound of formula (I): 1
    Type: Application
    Filed: April 11, 2003
    Publication date: February 12, 2004
    Inventors: Jean-Luc Fauchere, Jean-Claude Ortuno, Nigel Levens, Susana Chamorro, Jean Albert Boutin
  • Bicyclic imidazo-5-yl-amine derivatives
    Publication number: 20040023927
    Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, 1
    Type: Application
    Filed: August 5, 2003
    Publication date: February 5, 2004
    Applicant: Gruenenthal GmbH
    Inventors: Matthias Gerlach, Corinna Maul
  • 5-Aryltetrazole Compounds, compositions thereof, and uses therefor
    Publication number: 20040019208
    Abstract: The present invention relates to 5-Aryltetrazole compounds, compositions comprising a 5-Aryltetrazole compound, and methods for treating an inflammation disease, a reperfusion disease, hyperuricemia, gout, or tumor-lysis syndrome in an animal in need thereof comprising administering to the animal an effective amount of a 5-Aryltetrazole compound.
    Type: Application
    Filed: July 18, 2002
    Publication date: January 29, 2004
    Inventors: Alex Nivorozhkin, John Van Duzer, Andrew Salzman, Garry Southan, Siya Ram, Qi Zeng, Csaba Szabo
  • Agent for inhibition of cytokine production and agent for inhibition of cell adhesion
    Publication number: 20040014792
    Abstract: The present invention provides an agent for inhibiting cytokine production or cell adhesion, comprising at least one compound selected from the group consisting of thiazole derivatives represented by the following general formula: 1
    Type: Application
    Filed: April 29, 2003
    Publication date: January 22, 2004
    Applicant: Otsuka Pharmaceutical Co. Ltd.
    Inventors: Masatoshi Chihiro, TakayukI Matsuzaki, Hisashi Nagamoto, Goro Miyakoda, Shinobu Sueyoshi, Toyoki Mori, Kazuyoshi Kitano, Isao Takemura, Hiroshi Yamashita, Fujio Tabusa
  • Process for the preparation of 1,2,4-triazolin-5-one derivatives
    Patent number: 6673939
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R represents hydrogen, C1-10alkyl, haloC1-10alkyl or aryl; which are useful intermediates in the preparation of morpholine derivatives of formula (A). Compounds of formula (A) are useful as therapeutic agents.
    Type: Grant
    Filed: February 5, 2003
    Date of Patent: January 6, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Cameron John Cowden
  • PROCESS TO PRODUCE OXAZOLIDINONES
    Publication number: 20030216572
    Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)
    Type: Application
    Filed: April 24, 2003
    Publication date: November 20, 2003
    Applicant: Pharmacia & Upjohn Company
    Inventor: Bruce Allen Pearlman
  • Morpholine and thiomorpholine tachykinin receptor antagonists
    Patent number: 6638930
    Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: April 17, 2001
    Date of Patent: October 28, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
  • Disubstituted pyrazolines and triazolines as factor Xa inhibitors
    Patent number: 6630468
    Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II: or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing groups, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: June 26, 2002
    Date of Patent: October 7, 2003
    Inventor: Donald J. P. Pinto
  • Fatty acid synthase inhibitors
    Patent number: 6608059
    Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: August 19, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Robert A. Daines, Israil Pendrak
  • DPP IV inhibitors
    Publication number: 20030130281
    Abstract: The present invention relates to compounds of formula (I) 1
    Type: Application
    Filed: October 14, 2002
    Publication date: July 10, 2003
    Inventors: Markus Boehringer, Daniel Hunziker, Holger Kuehne, Bernd M. Loeffler, Ramakanth Sarabu, Hans P. Wessel
  • Polymorphic form of a tachykinin receptor antagonist
    Patent number: 6583142
    Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
    Type: Grant
    Filed: August 12, 2002
    Date of Patent: June 24, 2003
    Assignee: Merck & Co.
    Inventors: Louis Crocker, James McCauley
  • Method for producing 1-substituted-1,2,3- triazole derivative
    Publication number: 20030069419
    Abstract: A method for producing a compound of the formula: 1
    Type: Application
    Filed: April 19, 2002
    Publication date: April 10, 2003
    Inventors: Tomomi Ikemoto, Tatsuya Ito, Kiminori Tomimatsu, Yasuhiro Sawai, Hirohiko Nishiyama, Yasushi Isogami
  • Substituted quinolinecarboxamides as antiviral agents
    Patent number: 6544990
    Abstract: The present invention discloses disubstiuted 4-oxo-1,4-dihydro-3-quinolinecarboxamide derivatives. The compounds are useful as antiviral agents, in particular, as agents against viruses of the herpes family.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: April 8, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: Valerie A. Vaillancourt, Joseph Walter Strohbach, Audris Huang
  • Polymorphic form of a tachykinin receptor antagonist
    Publication number: 20030027825
    Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3- (S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
    Type: Application
    Filed: August 12, 2002
    Publication date: February 6, 2003
    Applicant: Merck & Co. Inc.
    Inventors: Louis Crocker, James Mccauley
  • Substituted 1-(4-aminophenyl)pyrazoles and their use as anti-inflammatory agents
    Patent number: 6506747
    Abstract: 1-(4-aminophenyl)pyrazoles optionally substituted on the 3- and 5-positions of the pyrazole ring and on the amino group at the 4-position of the phenyl ring are disclosed and described, which pyrazoles inhibit IL-2 production in T-lymphocytes.
    Type: Grant
    Filed: June 3, 1999
    Date of Patent: January 14, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashekhar Betageri, Charles L. Cywin, Karl Hargrave, Mary Ann Hoermann, Thomas M. Kirrane, Thomas M. Parks, Usha R. Patel, John R. Proudfoot, Rajiv Sharma, Sanxing Sun, Xiao-Jun Wang
  • Silver halide color photographic lightsensitive material and novel pyrrolotriazole compound
    Patent number: 6495697
    Abstract: A silver halide color photographic lightsensitive material contains a coupler represented by formula (I) below in at least one layer on a support (in this formula, X represents a hydrogen atom or a group which can split off by a coupling reaction with an oxidized form of an aromatic primary amine color developing agent, each of R1 and R2 represents an electron-attracting group having a Hammett's substituent constant p value of 0.20 or more, and the sum of the p values of R1 and R2 is 0.65 or more, and each of G1 and G2 represents a nitrogen atom or a substituent). A pyrrolotriazole compound represented by formula (I) below is also provided.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: December 17, 2002
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keiichi Tateishi, Hisashi Mikoshiba, Naoto Matsuda
  • Glucagon antagonists/inverse agonists
    Publication number: 20020187982
    Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.
    Type: Application
    Filed: November 16, 2001
    Publication date: December 12, 2002
    Inventors: Carsten Behrens, Jesper Lau, Peter Madsen
  • Bicyclic imidazo-5-yl-amine derivatives
    Publication number: 20020183320
    Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, 1
    Type: Application
    Filed: April 8, 2002
    Publication date: December 5, 2002
    Inventors: Matthias Gerlach, Corinna Maul
  • Novel compounds useful as neuro-protective agents
    Publication number: 20020177595
    Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
    Type: Application
    Filed: March 27, 2002
    Publication date: November 28, 2002
    Inventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
  • Pharmaceutical compositions and methods for use
    Publication number: 20020160998
    Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacylic compounds. The present invention relates in particular to five-membered heteroaromatic olefinic azacyclic compounds and five-membered heteroaromatic acetylenic azacylic compounds, including isoxazolyl olefinic cycloalkylamines and isoxazolyl acetylenic cycloalkylamines.
    Type: Application
    Filed: April 30, 2001
    Publication date: October 31, 2002
    Inventor: Thomas Jeffrey Clark
  • 3-ox(adi) azolylpropanohydroxamic acids useful as procollagen C- Proteinase inhibitors
    Publication number: 20020151535
    Abstract: Compounds of formula (I): 1
    Type: Application
    Filed: December 12, 2001
    Publication date: October 17, 2002
    Inventor: Usa Datta
  • Substituted 3,5-diphenyl-1,2,4-triazoles and their use as pharmaceutical metal chelators
    Patent number: 6465504
    Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: October 15, 2002
    Assignee: Novartis AG
    Inventors: René Lattmann, Pierre Acklin
  • 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
    Publication number: 20020137931
    Abstract: Compounds of formula I 1
    Type: Application
    Filed: January 11, 2002
    Publication date: September 26, 2002
    Inventors: Yousseff L. Bennani, Ramin Faghih, Wesley J. Dwight, Anil Vasudevan, Scott E. Conner
  • Polymorphic form of a tachykinin receptor antagonist
    Patent number: 6432952
    Abstract: This invention is concerned with a novel polymorphic forms of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethyl-amino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic forms have advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethylamino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
    Type: Grant
    Filed: October 26, 2000
    Date of Patent: August 13, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Louis Crocker, Dongwei Cai, Jiang Wang
  • Novel compounds
    Publication number: 20020086862
    Abstract: The invention provides certain 1,2,4-triazole-3-thione compounds, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 10, 2001
    Publication date: July 4, 2002
    Applicant: AstraZeneca AB
    Inventors: Andrew Baxter, Colin Bennion, Peter Cage, Nicholas Kindon, Michael Mortimore, Bryan Roberts
  • Tetrazolyl-phenyl actamide glucokinase activators
    Publication number: 20020065275
    Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.
    Type: Application
    Filed: January 16, 2002
    Publication date: May 30, 2002
    Inventor: Achyutharao Sidduri
  • Bicyclic amine derivatives
    Publication number: 20020061913
    Abstract: The present invention provides compounds of formula (I): 1
    Type: Application
    Filed: June 22, 2001
    Publication date: May 23, 2002
    Inventors: Christopher John Urch, Terence Lewis, Raymond Leo Sunley, Roger Salmon, Christopher Richard Ayles Godfrey, Christopher Ian Brightwell, Matthew Brian Hotson
  • 1H-pyrrolo-[1,2-b][1,2,4,]triazole compound and its synthetic intermediate, and method of preparing a 1H-1,2,4-triazole-5-yl-acetic acid ester compound
    Patent number: 6384219
    Abstract: There is disclosed a 1H-pyrrolo-[1,2-b][1,2,4]triazole compound represented by formula (I): wherein R is an alkyl group; R1, R2, R3, R1′, R2′, and R3′ each are a hydrogen atom or an alkyl group; R1 and R2, and R1′ and R2′ may bond together to form a ring, respectively; R4 is a hydrogen atom or an alkyl group, and X is heterocyclic group, a substituted amino group, or an aryl group. The compound is useful as a photographic cyan coupler. There is also disclosed synthetic intermediates of the compound and a production method of the intermediates.
    Type: Grant
    Filed: January 7, 1998
    Date of Patent: May 7, 2002
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Yasuhiro Shimada, Hideki Maeta, Yoshio Shimura
  • Substituted benzimidazoles
    Patent number: 6358978
    Abstract: Compounds of formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NF&kgr;B is involved.
    Type: Grant
    Filed: June 22, 2000
    Date of Patent: March 19, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Olaf Ritzeler, Hans Ulrich Stilz, Bernhard Neises, William Jerome Bock, Jr., Armin Walser, Gary A. Flynn, Jörg Habermann, Gerhard Jähne
  • Chemical synthesis of morpholine derivatives
    Publication number: 20020019524
    Abstract: 1
    Type: Application
    Filed: September 10, 2001
    Publication date: February 14, 2002
    Applicant: Merck Sharp & Dohme Limited
    Inventors: Ian Frank Cottrell, Ulf H. Dolling, David Hands, Robert Darrin Wilson
  • 1,2,4-triazole based compounds that can be used as insecticides or acaricides and processes
    Publication number: 20020019370
    Abstract: 3-(Substituted aryl)-5-{substituted aryl-(alkynyl-aryl)}-[1,2,4]- triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.
    Type: Application
    Filed: April 13, 2001
    Publication date: February 14, 2002
    Inventors: Vidyadhar Babu Hegde, Scott Jerome Bis, Emilie Chassat Heo, Christopher Thomas Hamilton, Peter Lee Johnson, Laura Lee Karr, Timothy Patrick Martin, Paul Allen Neese, Nailah Orr, Francis Eugene Tisdell, Maurice Chee Hoong Yap, Yuanming Zhu
  • Oxazolidinone antibacterial agents having a thiocarbonyl functionality
    Publication number: 20020016323
    Abstract: The present invention provides compounds of Formula 1 1
    Type: Application
    Filed: March 30, 2001
    Publication date: February 7, 2002
    Applicant: Pharmacia & Upjohn Company
    Inventors: Jackson B. Hester, Eldon George Nidy, Salvatore Charles Perricone, Toni-Jo Poel
  • Asymmetrical bisbenzotriazoles substituted by a perfluoroalkyl moiety and compositions stabilized therewith
    Patent number: 6337402
    Abstract: Asymmetrical bisbenzotriazoles of the formula I where G2′ is perfluoroalkyl of 1 to 12 carbon atoms, preferably CF3, and where G2 does not contain said group are red-shifted and due to the asymmetry are particularly soluble and useful in a host of applications including automotive coatings, thermoplastics and especially in adhesive compositions, themselves useful in solar panels and other laminate structures.
    Type: Grant
    Filed: January 22, 2001
    Date of Patent: January 8, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Mervin Wood, Jacqueline Lau, Ramanathan Ravichandran
  • Process for preparing 3-(substituted phenyl)-5-thienyl or furyl)-1,2,4-triazoles and novel intermediates utilized therein
    Patent number: 6329528
    Abstract: New synthetic procedures for preparing insecticidal 3-(substituted phenyl)-5-(thienyl or furyl)-1,2,4-triazoles utilizing thioimidate intermediate.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: December 11, 2001
    Assignee: Dow AgroSciences LLC
    Inventors: Mary L. Ash, Mark W. Zettler, Norman R. Pearson, Duane R. Romer, John W. Hull, Jr., David E. Podhorez
  • Polymorphic form of a tachykinin receptor antagonist
    Publication number: 20010041702
    Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,1-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
    Type: Application
    Filed: May 7, 2001
    Publication date: November 15, 2001
    Applicant: Merck & Co., Inc.
    Inventors: Louis Crocker, James Mccauley
  • Benzimidazole and its ribonucleoside
    Patent number: 6307043
    Abstract: The present invention relates to benzimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.
    Type: Grant
    Filed: January 21, 2000
    Date of Patent: October 23, 2001
    Assignee: Glaxo Wellcome Inc.
    Inventors: Stanley Dawes Chamberlain, Jeffrey H. Tidwell
  • Chemical synthesis of morpholine derivatives
    Patent number: 6297376
    Abstract: The present invention relates to a process for the preparation of mopholine derivatives of formula (I) which are useful as a therapeutic agents.
    Type: Grant
    Filed: December 15, 2000
    Date of Patent: October 2, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian Frank Cottrell, Ulf H Dolling, David Hands, Robert Darrin Wilson
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Patent number: 6294561
    Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: September 25, 2001
    Assignee: ICOS Corporation
    Inventors: Kerry W. Fowler, Joshua Odingo
  • Asymmetrical bisbenzotriazoles substituted by a perfluoroalkyl moiety
    Patent number: 6245915
    Abstract: Asymmetrical bis benzotriazoles of the formula I where G2′ is perfluoroalkyl of 1 to 12 carbon atoms, preferably CF3, and where G2 does not contain said group are red-shifted and due to the asymmetry are particularly soluble and useful in a host of applications including automotive coatings, thermoplastics and especially in adhesive compositions, themselves useful in solar panels and other laminate structures.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: June 12, 2001
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Mervin Wood, Jacqueline Lau, Ramanathan Ravichandran
  • Polymorphic form of a tachykinin receptor antagonist
    Patent number: 6229010
    Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
    Type: Grant
    Filed: December 9, 1999
    Date of Patent: May 8, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Louis Crocker, James McCauley
  • Benzotriazole UV absorbers having enhanced durability
    Patent number: 6166218
    Abstract: Benzotriazole UV absorbers which are substituted at the 5-position of the benzo ring by an electron withdrawing group exhibit enhanced durability and very low loss rates when incorporated into automotive coatings. This is particularly the case when the 3-position of the phenyl ring is also substituted by phenyl or phenylalkyl such as .alpha.-cumyl. Compounds where the 5-position of the benzo ring are substituted by perfluoroalkyl such as trifluoromethyl are particularly of interest for both their enhanced durability and for their excellent solubility and excellent color properties in some thermoplastic compositions when the phenyl ring is substituted at the 3-position by hydrogen or tert-alkyl.
    Type: Grant
    Filed: January 21, 1999
    Date of Patent: December 26, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Ramanathan Ravichandran, Joseph Suhadolnik, Mervin G. Wood, Anthony Debellis, Robert E. Detlefsen, Revathi Iyengar, Jean-Pierre Wolf
  • Cannabinoid receptor modulators
    Patent number: 6100259
    Abstract: Novel pyrazole derivatives are provided which are cannabinoid receptor modulators.
    Type: Grant
    Filed: October 15, 1999
    Date of Patent: August 8, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: Jia-Ning Xiang, John Duncan Elliott, Steven Todd Atkinson, Siegfried Benjamin Christensen, IV
  • One pot synthesis of 1,2,4-triazoles
    Patent number: 6096898
    Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: August 1, 2000
    Assignee: Dow AgroSciences LLC
    Inventors: David E. Podhorez, John W. Hull, Jr., Christine H. Brady
  • Polymorphic form of a tachykinin receptor antagonist
    Patent number: 6096742
    Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
    Type: Grant
    Filed: December 15, 1998
    Date of Patent: August 1, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Louis Crocker, James McCauley